Author/Editor		Wheatley, Mark; Hawtin, Stuart R; Howard, Helen C
Title		Neurohypophysial peptide hormone receptors: glycosylation, ligand recognition and effector coupling
Translated title		Receptorji nevrofizioloških peptidnih hormonov: glikozilacija, prepoznavanje ligandov in spojitev z efektorji
Type		članek
Source		Acta Biol Slov
Vol. and No.		Letnik 43, št. 1-2
Publication year		2000
Volume		str. 143-6
Language		eng
Abstract		The effects of the neurohypophysial peptide hormones vasopressin (AVP) and oxytocin (OT) are mediated by a family of related G-protein-coupled receptors. We have investigated the structure and function of these receptors using a combination of site-directed mutagenesis and recombinant expression in cultured HEK 293T cells. Receptor constructs were characterised pharmacologically using radioligand binding and second messenger assays. Data establish that ligand:receptor interaction involves extracellular domains and that a conserved acidic residue in transmembrane helix 2 is important for receptor activation. Using a cell-free translation system, the glycoprotein nature of the V1a subtype of vasopressin receptor is analysed and the importance of this glycosylation for efficient receptor expression is revealed. Overall, this study highllights the importance of certain residues within the receptor structure to normal receptor functioning.
Summary		Učinke nevrofizioloških peptidnih hormonov vazopresina (AVP) in oksitocina (OT) posreduje družina receptorjev, ki so sorodni receptorjem povezanim z G-proteini. V našem delu smo raziskovali odnos med strukturo in funkcijo omenjenih receptorjev s pomočjo usmerjene mutageneze in rekombinantne ekspresije v gojenih celicah HEK 293T. Farmakološke lastnosti dobljenih receptorjev smo proučevali tako, da smo jih izotopsko označili in nato uporabili test s sekundarnimi sporočevalci. Rezultati kažejo, da pri interakciji med ligandom in receptorjem sodelujejo zunaj membranske domene receptorja in da so ohranjeni kisli ostanki v 2. transmembranskem heliksu pomembni za aktivacijo receptorja. S pomočjo brezceličnega translacijskega sistema smo proučevali glikoproteinsko naravo receptorja vazopresinskega subtipa V1a, in ugotovili, da ima za uspešno ekspresijo receptorja pomembno vlogo sama glikozilacija proteina. Ugotovili smo, da so za pravilno delovanje receptorja pomembni nekateri aminokislinski ostanki.
Descriptors		CELL LINE RECEPTORS, PEPTIDE RADIOLIGAND ASSAY VASOPRESSINS OXYTOCIN